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ID: ALA3608239
Journal: Bioorg Med Chem Lett
Title: Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Authors: Fairhurst RA, Imbach-Weese P, Gerspacher M, Caravatti G, Furet P, Zoller T, Fritsch C, Haasen D, Trappe J, Guthy DA, Arz D, Wirth J.
Abstract: Exploring the affinity-pocket binding moiety of a 2-aminothiazole (S)-proline-amide-urea series of selective PI3Kα inhibitors using a parallel-synthesis approach led to the identification of a novel 4',5-bisthiazole sub-series. The synthesis and optimisation of both the affinity pocket and (S)-proline amide moieties within this 4',5-bisthiazole sub-series are described. From this work a number of analogues, including 14 (A66) and 24, were identified as potent and selective PI3Kα inhibitor in vitro tool compounds.
CiteXplore: 26206504